HIV-1 protease inhibition potential of functionalized polyoxometalates.

abstract：:Novel triazolopyrimidine acylsulfonamides class of antimycobacterial agents, which are mycobacterial acetohydroxyacid synthase (AHAS) inhibitors were designed by hybridization of known AHAS inhibitors such as sulfonyl urea and triazolopyrimidine sulfonamides. This Letter describes the synthesis and SAR studies of this...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patil V,Kale M,Raichurkar A,Bhaskar B,Prahlad D,Balganesh M,Nandan S,Shahul Hameed P

更新日期：2014-05-01 00:00:00

abstract：:Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58nM (K(i)) functional activity against the μ opioid receptor. DMPK da...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang C,Westaway SM,Speake JD,Bishop MJ,Goetz AS,Carballo LH,Hu M,Epperly AH

更新日期：2011-01-15 00:00:00

abstract：:The synthesis of amidinoaryloxy 9-benzyl-8-methyl-9H-purine, 7,8-dihydropteridine-6(5H)-one and 5,7-dihydropyrimido[4,5-b][1,4]oxazine-6-one inhibitors of Factor Xa is described. These compounds show nanomolar potency against FXa and maintain high selectivity over thrombin and trypsin. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Buckman BO,Mohan R,Koovakkat S,Liang A,Trinh L,Morrissey MM

更新日期：1998-08-18 00:00:00

abstract：:A novel cys-annexin A5 with a single cysteine-residue at its concave side has been developed by site-directed mutagenesis to allow conjugation through thiol-chemistry without affecting its apoptotic cell binding properties and was derivatized with HYNIC in a 1:1 stoichiometry. Similar to that of the 1st generation 99m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fonge H,de Saint Hubert M,Vunckx K,Rattat D,Nuyts J,Bormans G,Ni Y,Reutelingsperger C,Verbruggen A

更新日期：2008-07-01 00:00:00

abstract：:A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Seward EM,Carlson E,Harrison T,Haworth KR,Herbert R,Kelleher FJ,Kurtz MM,Moseley J,Owen SN,Owens AP,Sadowski SJ,Swain CJ,Williams BJ

更新日期：2002-09-16 00:00:00

abstract：:Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P(1) benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deaton DN,Gao EN,Graham KP,Gross JW,Miller AB,Strelow JM

更新日期：2008-01-15 00:00:00

abstract：:A novel class of HCV NS5B RNA dependent RNA polymerase inhibitors containing 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran scaffolds were designed and synthesized. Optimization of the alkyl substituent in the pyran ring showed preference for an n-propyl group, while 5,8-disubsti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gopalsamy A,Aplasca A,Ciszewski G,Park K,Ellingboe JW,Orlowski M,Feld B,Howe AY

更新日期：2006-01-15 00:00:00

abstract：:Tubulin is subject to a reversible post-translational modification involving polyglutamylation and deglutamylation of glutamate residues in its C-terminal tail. This process plays key roles in regulating the function of microtubule associated proteins, neuronal development, and metastatic progression. This study descr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu Y,Garnham CP,Roll-Mecak A,Tanner ME

更新日期：2013-08-01 00:00:00

abstract：:A series of 7-alkyl ether derivatives related to zanamivir were synthesized using direct alkylation of the C-7 alcohol of sialic acid. Alkyl ether moiety of less than 12 carbons in length showed low nanomolar inhibitory activity against influenza A virus sialidase. Furthermore, their moiety improved influenza A virus ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Honda T,Masuda T,Yoshida S,Arai M,Kaneko S,Yamashita M

更新日期：2002-08-05 00:00:00

abstract：:In order to obtain information regarding the design of selective DPP4 inhibitors, a 3D-QSAR study was conducted using DPP4, DPP8, and DPP9 inhibitors including newly synthesized six- and seven-membered cyclic hydrazine derivatives (KR64300, KR64301), which were evaluated in vitro for their inhibition of DPP4, DPP8, an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kang NS,Ahn JH,Kim SS,Chae CH,Yoo SE

更新日期：2007-07-01 00:00:00

abstract：:This article describes the syntheses and SAR of a series of imidazolopyrimidine derivatives, which are evaluated as inhibitors of PI3-Kinase (PI3K) and mTOR. These compounds were found to be ATP competitive with good tumor cell growth inhibition, and suppression of pathway specific biomakers such as phosphorylation of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkatesan AM,Dehnhardt CM,Chen Z,Santos ED,Dos Santos O,Bursavich M,Gilbert AM,Ellingboe JW,Ayral-Kaloustian S,Khafizova G,Brooijmans N,Mallon R,Hollander I,Feldberg L,Lucas J,Yu K,Gibbons J,Abraham R,Mansour TS

更新日期：2010-01-15 00:00:00

abstract：:Three novel metabolites of the angiotensin-II (A-II) receptor antagonist tasosartan have been identified in humans, and the syntheses and pharmacologic profiling of these metabolites are reported. Each metabolite bound the human A-II receptor with IC(50)s between 20 and 45nM. The in vivo effects of these compounds in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Elokdah HM,Friedrichs GS,Chai SY,Harrison BL,Primeau J,Chlenov M,Crandall DL

更新日期：2002-08-05 00:00:00

abstract：:A new glucuronylated prodrug of nornitrogen mustard, incorporating the same spacer group as the doxorubicin prodrug HMR 1826, has been prepared. Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Papot S,Combaud D,Bosslet K,Gerken M,Czech J,Gesson JP

更新日期：2000-08-21 00:00:00

abstract：:This study aims to develop novel azatyrosinamide compounds structurally modified from ras-specific antioncogenic azatyrosine. Analogues 4-15 were prepared and their inhibition on the growth of wild-type and ras-transformed NIH 3T3 cell lines was compared. Compound 12 was found to be the most active with IC50 16.5+/-2....

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang HP,Hwang TL,Lee O,Tseng YJ,Shu CY,Lee SJ

更新日期：2005-10-01 00:00:00

abstract：:Human serum albumin (HSA) was shown to mediate oligoribonucleotide cleavage. Nonenzymatic glycation of HSA decreased the ribonuclease-like activity of the protein. According to (31)P NMR data, both native and glycated albumins induced hydrolysis of RNA molecule through 2',3'-cyclophosphate intermediates. A feasible me...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gerasimova YV,Erchenko IA,Shakirov MM,Godovikova TS

更新日期：2008-08-15 00:00:00

abstract：:New analogues of the venerable antimalarial drug primaquine have been synthesized and bioassayed in vivo against Pneumocystis carinii, a life-threatening infection common among immunosuppressed patients. Two of these new compounds are significantly more active than primaquine itself, and provide new information for fu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Goodwin TE,Boylan CJ,Current WL,Byrd JC,Edwards CB,Fuller DA,Green JL,Larocca CD,Raney KD,Ross AS,Tucker WA

更新日期：2000-10-02 00:00:00

abstract：:A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gaudette F,Raeppel S,Nguyen H,Beaulieu N,Beaulieu C,Dupont I,Macleod AR,Besterman JM,Vaisburg A

更新日期：2010-02-01 00:00:00

abstract：:NAD(P)H-dependent oxidoreductases play important roles in biology. Recently, we reported that the luminescence lifetime of some Tb(3+) complexes is sensitive to NAD(P)H, and we used this phenomenon to detect activities of these enzymes. However, conventional time-resolved luminescence assays are susceptible to static ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Terai T,Ito H,Hanaoka K,Komatsu T,Ueno T,Nagano T,Urano Y

更新日期：2016-05-01 00:00:00

abstract：:The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in 1 can be replaced by a simple, substituted aromatic ring such as a toluene in 2. The resulting compounds exhibit subnanomolar ren...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lacombe P,Aspiotis R,Bayly C,Chen A,Dubé D,Fortin R,Gallant M,Juteau H,Liu S,McKay D,Roy P,Wu T

更新日期：2010-10-01 00:00:00

abstract：:Bioassay-guided fractionation of the EtOAc extract of the stem bark of Erythrina abyssinica (Leguminosae) resulted in the isolation of three new (1-3), along with 12 known (4-15) pterocarpan derivatives. Their chemical structures were determined by physicochemical and spectroscopic data analysis (IR, UV, [alpha](D), C...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen PH,Le TV,Thuong PT,Dao TT,Ndinteh DT,Mbafor JT,Kang KW,Oh WK

更新日期：2009-12-01 00:00:00

abstract：:The orexin 1 receptor (OX1R) antagonists carrying a morphinan skeleton such as YNT-707 (2) and YNT-1310 (3) showed potent and extremely high selective antagonistic activity against OX1R. In the course of our study of the essential structure of YNT-707 for high binding affinity against OX1R, we prepared derivatives of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saitoh T,Seki K,Nakajima R,Yamamoto N,Kutsumura N,Nagumo Y,Irukayama-Tomobe Y,Ogawa Y,Ishikawa Y,Tanimura R,Yanagisawa M,Nagase H

更新日期：2019-09-15 00:00:00

abstract：:A novel series of 3,5,6-trisubstituted pyrazolo[4,3-d]pyrimidin-7-one derivatives, especially 6-N-arylcarboxamidopyrazolo[4,3-d]pyrimidin-7-ones were synthesized and evaluated for their in vitro anticancer activities against various human cancer cell lines. The inhibitory activities for several kinases have also been ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Devegowda VN,Kim JH,Han KC,Yang EG,Choo H,Pae AN,Nam G,Choi KI

更新日期：2010-03-01 00:00:00

abstract：:The effects of PEGylation of glucose-dependent insulinotropic polypeptide (GIP) on potency and dipeptidyl peptidase IV (DPPIV) stability are reported. N-terminal modification of GIP(1-30) with 40 kDa polyethylene glycol (PEG) abrogates functional activity. In contrast, C-terminal PEGylation of GIP(1-30) maintains full...

journal_title：Bioorganic & medicinal chemistry letters

authors： Salhanick AI,Clairmont KB,Buckholz TM,Pellegrino CM,Ha S,Lumb KJ

更新日期：2005-09-15 00:00:00

abstract：:In this study, we synthesized a series of enantiomerically pure (2R,3S)-disubstituted tetrahydropyranes with diverse functional groups using known methodologies. In addition to the tert-butyl dimethyl silyl group, other common protecting groups for hydroxyl groups such as allyl, acetate, and benzoate were used to obta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Donadel OJ,Martín T,Martín VS,Villar J,Padrón JM

更新日期：2005-08-01 00:00:00

abstract：:Structure-activity relationships (SAR) of fused 1,2,4-triazolo[1,5-c ]pyrimidine were performed. Various substituents were introduced into the heterocyclic ring to improve the potency of adenosine A(3) receptor binding affinity and A(3)-selectivity against other subtypes. Potent and selective A(3) receptor antagonists...

journal_title：Bioorganic & medicinal chemistry letters

authors： Okamura T,Kurogi Y,Hashimoto K,Sato S,Nishikawa H,Kiryu K,Nagao Y

更新日期：2004-07-16 00:00:00

abstract：:An asymmetric synthesis of alpha-amino acids with novel beta-branched side chains has been implemented. The syntheses feature a p-toluenesulfinylimine induced chiral Strecker approach and were found to be applicable to the introduction of both aliphatic and aromatic beta-branched sidechains for preparation of previous...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang M,Porte A,Diamantidis G,Sogi K,Kubrak D,Resnick L,Mayer SC,Wang Z,Kreft AF,Harrison BL

更新日期：2007-05-01 00:00:00

abstract：:A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou G,Wu D,Hermel E,Balogh E,Gochin M

更新日期：2010-03-01 00:00:00

abstract：:In the search of molecules that can serve as leads in the design of a new drug for the treatment of Chagas' disease, we found that some brevifolin carboxylate derivatives isolated from Geranium bellum Rose, inactivate triosephosphate isomerase from Trypanosoma cruzi (TcTIM) in a species-specific manner. After spectros...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gayosso-De-Lucio J,Torres-Valencia M,Rojo-Domínguez A,Nájera-Peña H,Aguirre-López B,Salas-Pacheco J,Avitia-Domínguez C,Téllez-Valencia A

更新日期：2009-10-15 00:00:00

abstract：:Benzothiazole benzimidazole (S)-isothiazolidinone ((S)-IZD) derivatives 5 were discovered through a peptidomimetic modification of the tripeptide (S)-IZD protein tyrosine phosphatase 1B (PTP1B) inhibitor 1. These derivatives are potent, competitive, and reversible inhibitors of PTP1B with improved caco-2 permeability....

journal_title：Bioorganic & medicinal chemistry letters

authors： Sparks RB,Polam P,Zhu W,Crawley ML,Takvorian A,McLaughlin E,Wei M,Ala PJ,Gonneville L,Taylor N,Li Y,Wynn R,Burn TC,Liu PC,Combs AP

更新日期：2007-02-01 00:00:00

abstract：:Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu H,Cui K,Wang L,Gou S

更新日期：2005-11-15 00:00:00